Method for e3nhanced delivery of oxybutynin and compositions thereof

#1. Field of the Invention

#This invention relates to compositions for enhancement of delivery of oxubutynin, antimuscarinic and spasmolytic drugs, by administration via the nasal route to treat patients suffering from overactive bladder with symptoms of urinary urgency, frequency or urge incontinence. The invention is also directed to methods of treatment thereof, and methods of preparation thereof.

#2. Description of the Related Art

#FIG. 1. depicts the structures of oxybutynin and its major metabolite N-desethyloxybutynin.

#FIG. 2 is a bar graph of oxybutynin (5 mg/kg) bioavailability in rats following nasal and oral administration, relative to the intravenous administration (100%). Data presented as mean±SEM (n=4).

#Orally administered oxybutynin currently available on the market show extensive first pass metabolism with a ten-fold variation between subjects. Thus, the present inventions have discovered a novel composition and method for the delivery of oxybutynin to a patient in need of such treatment, comprising the intranasal administration of oxybutynin. This composition and method offers significant clinical advantages over the prior art. More specifically, the inventors sought to provide a safe, effective, fast and convenient treatment for administering oxybutynin to a patient in need of such treatment, which comprises the administration of oxybutynin intranasally, thus avoiding the side-effects and other disadvantages associated with oral dosage forms. Specifically, smaller doses of oxybutynin can be administered through the nasal route, thus resulting in rapid onset of action, fewer side effects and reducing drug-drug interactions. By using the composition and method of the present invention, the drug will become more tolerable and more effective in treating patients suffering from overactive bladder with symptoms of urinary urgency, frequency or urge incontinence.

#Intranasal administration of oxybutynin is as effective as oral administration, but may be conveniently and painlessly self-administered by the patient, and at lower doses and faster onset of action compared to oral dosage forms, thereby allowing a decreased incidence of side effects and decreased incidence of drug-drug interactions and faster onset of action compared to the oral administration.

#As used in the present invention, the term “oxybutynin” will be understood to refer to either (R)-oxybutynin, (S)-oxybutynin, or a racemic mixture of (R)- and (S)-oxybutynin.